Talaaga

Thalidomide na faʻalauiloaina e avea o se vailaʻau faʻamalo, immunomodulatory agent ma o loʻo suʻesuʻeina foi mo le togafitia o faʻamaoniga o le tele o kanesa. Thalidomide faʻalavelaveina se E3 ubiquitin ligase,lea ose CRBN-DDB1-Cul4A lavelave.

Fa'amatalaga

O le Thalidomide o loʻo faʻalauiloaina muamua e avea ma sedative, faʻalavelaveina le cereblon (CRBN), o se vaega o le cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, faʻatasi ai ma le Kd o∼250 nM, ma ei ai immunomodulatory, anti-inflammatory ma anti-angiogenic meatotino o le kanesa.

I Vitro

O le Thalidomide o loʻo faʻalauiloaina muamua e avea o se faʻamaʻi, e iai le immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties, ma taulaʻi le cereblon (CRBN), o se vaega o le cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, ma le Kd o∼250 nM[1]. Talidomide (50μg / mL) faʻamalosia le gaioiga anti-tumour o le icotinib e faasaga i le faʻateleina o sela PC9 ma A549, ma o lenei aʻafiaga e fesoʻotaʻi ma apoptosis ma le femalagaiga o sela. E le gata i lea, o le Thalidomide ma le icotinib e faʻalavelaveina le EGFR ma le VEGF-R2 auala i sela PC9 [3].

Thalidomide (100 mg/kg, po) fa'alavelaveina le tu'uina atu o collagen, fa'alalo-fa'atonutonu le maualuga o fa'amatalaga mRNA oα-SMA ma le collagen I, ma faʻaititia tele le cytokines pro-inflammatory i isumu RILF. O le Thalidomide e faʻaitiitia ai le RILF e ala i le taofiofia o le ROS ma lalo ole tulafono faatonutonu ole TGF-β/ Smad ala fa'alagolago ile tulaga Nrf2[2]. Thalidomide (200 mg / kg, po) faʻatasi ma le icotinib o loʻo faʻaalia ai le synergistic anti-tumor aʻafiaga i isumu mataʻutia o loʻo i ai sela PC9, taofiofia le tuputupu aʻe o le tuma ma faʻateleina le oti [3].